Enteric Coated Adenosine A2A Antagonist Tablets
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Solution Overview
Problem
Current immunotherapy approaches for cancer face challenges in effectively targeting cancer cells due to elevated adenosine levels, which dampen the immune response and hinder the presentation of tumor antigens, necessitating improved formulations of adenosine A2A receptor antagonists with enhanced bioavailability, stability, and reduced gastric irritation.
Innovation Solution
Development of pharmaceutical compositions comprising micronized adenosine A2A receptor antagonist particles with specific size distributions and combinations of pharmaceutically acceptable excipients, such as polyols, disintegrants, and binders, formulated into tablets, capsules, granules, or powders, to optimize bioavailability, stability, and delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If adenosine A2A receptor antagonists are administered to treat cancer, then therapeutic efficacy is improved, but gastric irritation occurs
Solution Approach 1:
The patent introduces an enteric coating as an intermediary layer between the adenosine A2A receptor antagonist and the gastric environment. This coating acts as a mediator that protects the stomach from direct contact with the irritating drug while allowing the drug to reach its target in the intestine, thereby resolving the contradiction between therapeutic efficacy and gastric irritation
Solution Approach 2:
The patent applies a flexible enteric coating film to the tablet surface that selectively dissolves at specific pH levels. This thin film provides protection in the acidic gastric environment while allowing drug release in the more neutral intestinal environment, thus eliminating gastric irritation without compromising therapeutic efficacy
2Productivity
If micronized particles are used to improve bioavailability, then dissolution rate is improved, but manufacturing complexity increases
Solution Approach 1:
The patent performs micronization as a preliminary action during the drug formulation process, creating fine particles before tablet compression. This preliminary size reduction improves bioavailability and dissolution rate while the subsequent standard tabletting process with enteric coating maintains manufacturing feasibility by using conventional equipment and procedures
3Object-affected harmful factors
If enteric coating is applied to reduce gastric irritation, then gastric safety is improved, but drug release time is delayed
Solution Approach 1:
The patent utilizes pH parameter changes along the gastrointestinal tract to trigger drug release. The enteric coating is designed to remain intact in the acidic stomach environment (pH 1-3) and rapidly dissolve when encountering the more neutral pH conditions of the intestine (pH 6-7.4), thus providing gastric protection while ensuring timely drug release at the appropriate location
Solution Approach 2:
The patent employs commercially available enteric coating materials that have been extensively studied and validated for their pH-dependent release properties. By using established coating systems rather than developing novel release mechanisms, the patent achieves reliable gastric protection with predictable and timely drug release characteristics
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The compositions demonstrate superior bioavailability, stability, and pharmacokinetic properties, including rapid dissolution and disintegration, effectively enhancing the therapeutic efficacy of adenosine A2A receptor antagonists in treating various cancers.
Implementation Method 1
rapid dissolution and disintegration
Implementation Method 2
as measured by laser diffraction spectroscopy
Data Source
AI summary
The disclosure provides, inter alia, pharmaceutical compositions comprising micronized drug particles of adenosine A2A receptor antagonists, and methods of treating cancer using the pharmaceutical compositions.